Abstract: Disclosed herein are novel catalysts for producing remdesivir in one-pot manner, in which a diastereomerically enriched form of an intermediate, which following acidic hydrolysis would give rise to the desired remdesivir, was produced with the aid of the disclosed novel catalysts. Also disclosed herein is an improved process for the preparation of remdesivir without the need to separate one of the enantiomers while minimizing the formation of undesired isomers, thus offers economic advantages for operation on a commercial scale.

Abstract: The present disclosure provides a method for detecting cholangiocarcinoma cells. The capture rate of the cholangiocarcinoma cells of the present disclosure is higher than 70%, and a plurality of octasaccharides with high affinity and specificity can be modified on the surface of magnetic beads to capture and analyze cholangiocarcinoma cells under test, wherein the cholangiocarcinoma cells can be circulating tumor cells in cholangiocarcinoma.

Abstract: Disclosed herein is a novel compound of formula (I) for detecting circulating cancerous cells, particularly, cholangio-cancerous cells, from a biological sample, wherein, R1 and R2 are independently H, or —SO3M; and M is a monovalent cation selected from the group consisting of sodium ion, potassium ion, lithium ion or ammonium ion. Also disclosed herein is a method of treating and detecting cholangio-cancerous cells from a biological sample of a subject suspected of having cholangiocarcinoma (CCA). The method includes steps of, contacting the biological sample with a magnetic bead pre-coated with the compound of formula (I); detecting a complex formed between the magnetic bead and the biological sample in an immunoassay; and administering to the subject an effective amount of a chemotherapeutic agent to ameliorate symptoms associated with the CCA.

Abstract: Disclosed herein is a novel compound of formula (I) for detecting circulating cancerous cells, particularly, cholangio-cancerous cells, from a biological sample, wherein, R1 and R2 are independently H, or —SO3M; and M is a monovalent cation selected from the group consisting of sodium ion, potassium ion, lithium ion or ammonium ion. Also disclosed herein is a method of treating and detecting cholangio-cancerous cells from a biological sample of a subject suspected of having cholangiocarcinoma (CCA). The method includes steps of, contacting the biological sample with a magnetic bead pre-coated with the compound of formula (I); detecting a complex formed between the magnetic bead and the biological sample in an immunoassay; and administering to the subject an effective amount of a chemotherapeutic agent to ameliorate symptoms associated with the CCA.

Abstract: Disclosed herein are substrates and/or inhibitors of endo-O-sulfatase 1 (Sulf-1). According to some embodiments, the substrates and/or inhibitors of Sulf-1 are compounds of formula (I) or (II), In formula (I) or (II), n is 2 or 3; X is methylene, O, or N; R1 is —SO3M, or —SO2NH2; R2 is C1-6 alkyl or C1-6 alkylamine; and M is a monovalent cation selected from the group consisting of lithium, sodium, potassium, and ammonium. Also encompasses herein are methods of identifying and treating a subject having or suspected of having osteoarthritis.

Abstract: Disclosed herein is a sulfated octasacchande of formula (I), a pharmaceutically acceptable salt, solvate or ester thereof: wherein R1 is —NHAc or —NHSO3H; and R2 and R3 are independently H, or —SO3H. Also encompasses herein is a method of treating neuron injury and/or diseases associated with a disrupted autophagy flux. The method includes administering an effective amount of the sulfated octasaccharide of formula (I) to a subject in need of such treatment.

Abstract: Disclosed herein is a sulfated octasacchande of formula (I), a pharmaceutically acceptable salt, solvate or ester thereof: wherein R1 is —NHAc or —NHSO3H; and R2 and R3 are independently H, or —SO3H. Also encompasses herein is a method of treating neuron injury and/or diseases associated with a autophagy flux. The method includes administering an effective amount of the sulfated octasaccharide of formula (I) to a subject in need of such treatment.

Abstract: Disclosed herein is an integrated microfluidic chip for detecting cancerous cells, particularly, cholangio-cancerous cells, from a biological sample. Also disclosed herein is a method of detecting cholangio-cancerous cells from a biological sample.

Abstract: The present disclosure provides a method for detecting cholangiocarcinoma cells. The capture rate of the cholangiocarcinoma cells of the present disclosure is higher than 70%, and a plurality of octasaccharides with high affinity and specificity can be modified on the surface of magnetic beads to capture and analyze cholangiocarcinoma cells under test, wherein the cholangiocarcinoma cells can be circulating tumor cells in cholangiocarcinoma.

Abstract: The present invention relates to methods for the synthesis of fondaparinux and intermediates thereto.

Abstract: The present invention relates to methods for the synthesis of fondaparinux and intermediates thereto.

Abstract: The present invention relates to methods for the synthesis of fondaparinux and intermediates thereto.

Abstract: A method for preparing hexose derivatives comprises the steps of providing a silylated hexose, treating the silylated hexose with a first carbonyl compound in the presence of a catalyst to form an ketalized hexose, treating the ketalized hexose with a second carbonyl compound followed by treating with a first reductant to form an etherized hexose, and converting the etherized hexose into a target hexose derivative, which can be 2-alcohol hexose, 3-alcohol hexose, 4-alcohol hexose, or a 6-alcohol hexose. In particular, the present invention can prepare the hexose derivatives with highly regioselective scheme to protect individual hydroxyls of monosaccharide units and install an orthogonal protecting group pattern in a one-pot manner.

Abstract: Orthogonally protected disaccharide building blocks for synthesis of heparin saccharide are disclosed. The disaccharide building block has a formula (I), in which L is a leaving group, P1, P2, P3 and P4 are different, and of them P1 is an ester-type protecting group, P2 is a hydroxyl protecting group that could be oxidized to a carboxylic acid, P3 is a hydroxyl protecting group, and P4 is a hydroxyl protecting group which allows chemoselective deprotection with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). Acting as an elongation unit, the disaccharide building block of formula (I) may react with a starting unit of formula (II) to synthesize a heparin saccharide of desired size.

Abstract: Orthogonally protected disaccharide building blocks for synthesis of heparin oligosaccharide. The disaccharide building block has a formula (I), in which L is a leaving group, P1, P2, P3 and are different, and of them P1 is an ester-type protecting group, P2 is a hydroxyl protecting group that could be oxidized to a carboxylic acid, P3 is a hydroxyl protecting group, and P4 is a hydroxyl protecting group which allows chemoslective deprotection with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). Acting as an elongation unit, the disaccharide building block of formula (I) may react with a starting unit of formula (II) to synthesize a heparin oligosaccharide.

Abstract: Disaccharide compounds used as building blocks for making heparin and heparan sulfate oligosaccharides. Also disclosed are methods for making these disaccharide compounds.

Abstract: A method for preparing hexose derivatives comprises the steps of providing a silylated hexose, treating the silylated hexose with a first carbonyl compound in the presence of a catalyst to form an ketalized hexose, treating the ketalized hexose with a second carbonyl compound followed by treating with a first reductant to form an etherized hexose, and converting the etherized hexose into a target hexose derivative, which can be 2-alcohol hexose, 3-alcohol hexose, 4-alcohol hexose, or a 6-alcohol hexose.

Abstract: The present invention provides composition and methods for the synthesis of low molecular weight heparins and heparinoids. The present invention also provides compositions having substantially homogenous populations of desired heparin molecules, or molecules useful in the synthesis of heparin oligosaccharides.

Abstract: The present invention provides composition and methods for the synthesis of low molecular weight heparins and heparinoids. The present invention also provides compositions having substantially homogenous populations of desired heparin molecules, or molecules useful in the synthesis of heparin oligosaccharides.

Abstract: The invention relates to a method of preparing a compound of the following formula: wherein each of R1, R2, R3, and R4, independently, is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, alkoxy, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, or alkyloxyalkyl, provided that R1 and R2, optionally form a keto or, with the carbon atom to which they are attached, optionally form a cyclic moiety, and that R3 and R41, optionally form a keto or, with the carbon atom to which they are attached, optionally form a cyclic moiety.